Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens
ElAwamy, Moustafa; Mohammad, Haroon; Hussien, Abdelrahman; Abutaleb, Nader S; Hagras, Mohamed; Serya, Rabah; Taher, Azza T; Seleem, Mohamed N; Mayhoub, Abdelrahman S; Khaled A M Abouzid;
Abstract
With the continued rise of antibiotic resistance and reduced susceptibility to almost all front-line antibiotics, multidrug-resistant Gram-positive bacterial infections represent an incessant threat to healthcare providers. This study presents a new series of phenylthiazole compounds where two active moieties were combined into one scaffold. The antibacterial activity of the hybrid structures extended to include several clinically-relevant multi-drug resistant pathogens including methicillin-resistant and vancomycin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, vancomycin-resistant enterococci, cephalosporin-resistant and methicillin-resistant Streptococcus pneumoniae, and Listeria monocytogenes. In addition, the most potent compounds, 16a and 17a, exhibited a fast bactericidal mode of action in vitro with low susceptibility to induce bacterial resistance. In addition to its potent spectrum of activity against Gram-positive bacterial pathogens, compound 17a was found to be metabolically stable in rats, with a half-life of 4 h.
Other data
Title | Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens | Authors | ElAwamy, Moustafa; Mohammad, Haroon; Hussien, Abdelrahman; Abutaleb, Nader S; Hagras, Mohamed; Serya, Rabah ; Taher, Azza T; Seleem, Mohamed N; Mayhoub, Abdelrahman S; Khaled A M Abouzid | Keywords | Antibiotic resistance;Methicillin-resistant Staphylococcus aureus (MRSA);Pharmacokinetics;Vancomycin-resistant Enterococci (VRE) | Issue Date | 25-May-2018 | Publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | Journal | European Journal of Medicinal Chemistry | Volume | 152 | Start page | 318 | End page | 328 | ISSN | 0223-5234 | DOI | 10.1016/j.ejmech.2018.04.049 | PubMed ID | 29734000 | Scopus ID | 2-s2.0-85046620319 | Web of science ID | WOS:000435048900026 |
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